Bedaquinline

Bedaquiline is a pivotal pharmaceutical active ingredient and reference standard used in the treatment of multidrug-resistant tuberculosis (MDR-TB). As the active pharmaceutical ingredient in Sirturo® (bedaquiline fumarate), Bedaquiline is indicated for use in combination therapy for pulmonary MDR-TB in adults. Bedaquiline functions as a mycobacterial ATP synthase inhibitor, binding to both the c-subunit and the ε-subunit of the enzyme, thereby depleting cellular energy and leading to bacterial cell death. As a key reference material, Bedaquiline is essential for analytical method development, impurity profiling, and quality control testing in generic manufacturing and ANDA filings. The compound's unique diarylquinoline scaffold has also attracted interest in drug discovery programs targeting other infectious diseases and has been investigated for its potential against SARS-CoV-2 3CL protease. Bedaquiline is supplied with detailed characterization data compliant with regulatory guidelines, making it an indispensable tool for pharmaceutical research and development.

 

Product Parameters

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Parameter	Specification
Product Name	Bedaquiline
CAS Number	843663-66-1
Molecular Formula	C₃₂H₃₁BrN₂O₂
Molecular Weight	555.50 g/mol
Appearance	White solid
Melting Point	104℃
Boiling Point	702.7±60.0℃
Solubility	Soluble in DMSO (10 mg/mL)
Storage Condition	Room temperature

 

Pharmacological Action

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Bedaquiline exhibits equivalent bactericidal activity against both sensitive and drug-resistant strains of Mycobacterium tuberculosis, as well as significant sterilizing effects on dormant bacteria.

 

Mechanism Of Action

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The unique and specific anti-tuberculosis (TB) target of bedaquiline is the proton pump of Mycobacterium tuberculosis ATP synthase. ATP synthase is the key enzyme for ATP synthesis in Mycobacterium tuberculosis. When the oligomer of ATP synthase and lipoprotein subunit c bind to bedaquiline, they inhibit ATP synthesis, leading to bacterial death. Compared with existing anti-TB drugs, bedaquiline exhibits a novel anti-TB mechanism and does not induce cross-resistance with current tubercular agents. The gene sequence encoding subunit c of ATP synthase is designated atpE, and its amino acid sequence is highly conserved. Resistance to bedaquiline in Mycobacterium tuberculosis arises from mutations at positions 63 or 66 of the atpE gene, which impair bedaquiline's binding affinity to the ATP synthase c subunit.

 

Pharmacokinetics

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Bedaquiline is well absorbed orally, with its bioavailability being twice that of fasting conditions when taken with food. It reaches peak plasma concentrations at 5 hours, exhibits a plasma protein binding rate exceeding 99.9%, and has a plasma half-life of 173 hours. It is widely distributed in tissues, with a steady-state distribution volume exceeding 1000 L, low clearance, and an elimination half-life of 5.5 months. Bedaquiline is primarily demethylated by CYP3A4, with partial metabolism via CYP2C8 and CYP2C19 to metabolites 1–8, the most prominent being the demethylated product M2. The biological activity of M2 is only 1/3 to 1/6 that of bedaquiline, but it demonstrates stronger cytotoxicity and a higher propensity for drug-induced phospholipid disorders. The majority of bedaquiline and its metabolites are excreted via feces, while only 1%–4% are eliminated in urine.

 

Contact Us

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Need Bedaquiline for your MDR-TB API manufacturing campaign, impurity profiling program, or drug discovery research? Cosperpharm makes it straightforward. Reach out to our team for pricing, documentation, or technical support—we're here to help you move your project forward.